Patents Examined by D. Dinner
  • Patent number: 4771054
    Abstract: Novel quinoline-carboxylic acids as antibacterial agents are described as well as methods for their manufacture, formulation, and use in treating bacterial infections including the description of certain novel intermediates used in the manufacture of the antibacterial agents.
    Type: Grant
    Filed: August 15, 1986
    Date of Patent: September 13, 1988
    Assignee: Warner-Lambert Company
    Inventors: John M. Domagala, Thomas F. Mich, Jeffrey B. Nichols
  • Patent number: 4765974
    Abstract: A clonidine preparation for percutaneous administration comprising a support having provided thereon an active ingredient-containing layer is disclosed. The active ingredient-containing layer contains an acrylic polymer having a glass transition temperature of from -70.degree. C. to -10.degree. C. and pressure-sensitive adhesion at room temperature as a base, at least one of clonidine and clonidine hydrochloride as an active ingredient, and a decomposition inhibitor. The active ingredient can be stably maintained within the preparation without being decomposed, and, therefore, can be effectively released over a prolonged period of time.
    Type: Grant
    Filed: May 13, 1987
    Date of Patent: August 23, 1988
    Assignee: Nitto Electric Industrial Co., Ltd.
    Inventors: Shoichi Tokuda, Yuusuke Ito, Saburo Otsuka, Takashi Kinoshita
  • Patent number: 4758670
    Abstract: Fluoroazolylpropane derivatives of the formula I ##STR1## are described, in which Az is imidazolyl or triazolyl, R.sup.1 is hydrogen, alkyl or aralkyl which is unsubstituted or substituted by halogen, alkyl, alkoxy, halogenoalkyl, nitro, cyano, carboxyl or alkoxycarbonyl, R.sup.2 is C.sub.1 -C.sub.10 -alkyl which is unsubstituted or substituted by alkoxy, aralkoxy or phenyl, it being possible for the aromatic nuclei of aralkoxy and phenyl in turn to be unsubstituted or substituted by halogen, alkyl, alkoxy, halogenoalkyl, cyano, carboxyl or alkoxycarbonyl, R.sup.3 is hydrogen, alkyl, alkylcarbonyl or aralkyl which is unsubstituted or substituted by halogen, alkoxy, alkyl, halogenoalkyl, cyano, carboxyl or alkoxycarbonyl, R.sup.5 is an unsubstituted or monosubstituted or polysubstituted radical selected from the series comprising C.sub.1 -C.sub.8 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.
    Type: Grant
    Filed: January 4, 1984
    Date of Patent: July 19, 1988
    Assignee: Ciba-Geigy Corporation
    Inventors: Urs Muller, Hermann Rempfler, Hans Tobler
  • Patent number: 4749405
    Abstract: 1-Vinyltriazole compounds of the formula ##STR1## wherein R.sup.1 is alkyl, substituted alkyl, cycloalkyl, aryl or substituted aryl;R.sup.2 is alkyl;R.sup.3 is alkyl, cycloalkyl, cycloalkenyl, substituted cycloalkenyl, alkenyl, aryl or substituted aryl; orR.sup.2 and R.sup.3, together with the carbon to which they are bonded, represent cycloalkenyl, substituted cycloalkenyl, cycloalkyl or substituted cycloalkyl;is the group ##STR2## or, alternatively, X may represent a keto group provided that when X is a keto group, R.sup.1 is alkyl, substituted alkyl, cycloalkyl, or substituted cycloalkyl;R.sup.4 is hydrogen, alkyl, aralkyl, substituted aralkyl, acyl, carbamoyl or substituted carbamoyl;R.sup.5 is hydrogen, alkyl, aralkyl or substituted aralkyl;and acid addition salts and metal salt complexes thereof; are outstandingly effective plant growth regulants and as fungicides.
    Type: Grant
    Filed: August 8, 1986
    Date of Patent: June 7, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Wolf Reiser, Wilfried Draber, Karl H. Buchel, Klaus Lurssen, Paul-Ernst Frohberger, Volker Paul
  • Patent number: 4743293
    Abstract: 1-Vinyltriazole compounds of the formula ##STR1## wherein R.sup.1 is alkyl, substituted alkyl, cycloalkyl, aryl or substituted aryl;R.sup.2 is alkyl;R.sup.3 is alkyl, cycloalkyl, cycloalkenyl, substituted cycloalkenyl, alkenyl, aryl or substituted aryl; orR.sup.2 and R.sup.3, together with the carbon to which they are bonded, represent cycloalkenyl, substituted cycloalkenyl, cycloalkyl or substituted cycloalkyl;X is the group ##STR2## or, alternatively, X may represent a keto group provided that when X is a keto group, R.sup.1 is alkyl, substituted alkyl, cycloalkyl, or substituted cycloalkyl;R.sup.4 is hydrogen, alkyl, aralkyl, substituted aralkyl, acyl, carbamoyl or substituted carbamoyl;R.sup.5 is hydrogen, alkyl, aralkyl or substituted aralkyl;and acid addition salts and metal salt complexes thereof;are outstandingly effective plant growth regulants and as fungicides.
    Type: Grant
    Filed: July 30, 1986
    Date of Patent: May 10, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Wolf Reiser, Wilfried Draber, Karl H. Buchel, Klaus Lurssen, Paul-Ernst Frohberger, Volker Paul
  • Patent number: 4737497
    Abstract: Disclosed are novel bis-dioxopiperazine derivatives, process for their preparation, antitumor agents comprising them and compositions containing them.The bis-dioxopiperazine derivatives are represented by the following general formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms; R.sub.2 represents a hydrogen atom or a group of ##STR2## R.sub.3 and R.sub.4, which are respectively independent and are the same or different, represent respectively a lower alkyl group having 1 to 4 carbon atoms, a cycloalkyl group having 3 to 7 carbon atoms or a heterocyclic radical selected from the group consisting of substituted or unsubstituted piperidino, substituted or unsubstituted piperazino, substituted or unsubstituted morpholino and substituted or unsubstituted thiomorpholino, or R.sub.3 and R.sub.
    Type: Grant
    Filed: April 4, 1984
    Date of Patent: April 12, 1988
    Assignee: Zenyaki Kogyo Kabushiki Kaisha
    Inventor: Yun-feng Ren
  • Patent number: 4703128
    Abstract: The feature of the present invention is a process for preparing compounds represented by general formula (Ia) described below: ##STR1## wherein X.sub.1, X.sub.2, X.sub.3, R.sub.1, R.sub.2, R.sub.3 and R.sub.7 are as defined in formula (I) and R.sub.10 represents a lower alkyl group, or acid salts thereof, which process is characterized by using the guanidylfungins (II) as raw materials, reacting these guanidylfungins with alcohols (III) in the presence of an acid catalyst, and then hydrolyzing the malonic acid monoester (IV).
    Type: Grant
    Filed: July 18, 1986
    Date of Patent: October 27, 1987
    Assignee: Takahara Shuzo Co., Ltd.
    Inventors: Teruhiko Beppu, Kazutoh Takesako, Teruya Nakamura, Akira Obayashi
  • Patent number: 4699777
    Abstract: A topical albuterol composition having superior transdermal flux containing various amounts of albuterol, 1-dodecyl-azacycloheptan-2-one and urea in a non-aqueous environment. The enhancement observed in albuterol skin penetration indicates that a therapeutically effective amount of albuterol can be delivered through skin using these formulations. The compositions can be administered topically as a cream, lotion or via a transdermal device.
    Type: Grant
    Filed: August 21, 1985
    Date of Patent: October 13, 1987
    Assignee: Schering Corporation
    Inventors: Michael A. Zupon, Joel A. Sequeira
  • Patent number: 4696945
    Abstract: The invention relates to parasiticidally and insecticidally highly active compounds of formula I ##STR1## wherein R.sub.1 is hydrogen or a protecting group;R.sub.2 is methyl, ethyl, isopropyl or sec-butyl; andR is a radical R.sub.3 which is bound through oxygen or sulfur and is selected from the group consisting of C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 haloalkyl, C.sub.1 -C.sub.10 hydroxyalkyl, C.sub.1 -C.sub.10 mercaptoalkyl, C.sub.2 -C.sub.10 alkoxyalkyl, C.sub.3 -C.sub.10 alkoxyalkoxyalkyl, hydroxy- or mercapto-substituted C.sub.3 -C.sub.10 alkoxyalkyl, C.sub.4 -C.sub.15 alkoxyalkoxyalkoxyalky, hdroxy- or mercapto-substituted C.sub.4 -C.sub.15 alkoxyalkoxyalkoxyalkyl, C.sub.2 -C.sub.10 -alkenyl, C.sub.2 -C.sub.10 haloalkenyl, C.sub.2 -C.sub.10 alkynyl, C.sub.2 -C.sub.10 haloalkynyl, phenyl which is unsubstituted or substituted by halogen, C.sub.1 -C.sub.3 -alkyl, C.sub.1 -C.sub.3 haloalkyl, C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.
    Type: Grant
    Filed: July 14, 1986
    Date of Patent: September 29, 1987
    Assignee: Ciba-Geigy Corporation
    Inventors: Bruno Frei, Anthony C. O'Sullivan
  • Patent number: 4684392
    Abstract: New substituted .beta.-triazolyl oximes, processes for their manufacture, agents for regulating plant growth containing these compounds, and a process for regulating plant growth with these compounds.
    Type: Grant
    Filed: January 9, 1985
    Date of Patent: August 4, 1987
    Assignee: BASF Aktiengesellschaft
    Inventors: Costin Rentzea, Hubert Sauter, Bernd Zeeh, Gerd Heilen, Johann Jung
  • Patent number: 4670454
    Abstract: Azolylmethylcycloalkanes of the formula I ##STR1## where A and B are identical or different and are each hydrogen, unsubstituted or halogen-substituted alkyl of 1 to 4 carbon atoms, naphthyl, hetaryl, biphenyl or phenyl, where the phenyl radical can be substituted by halogen, nitro, alkyl, alkoxy or haloalkyl, each of 1 to 4 carbon atoms, phenoxy or phenylsulfenyl, D and E are identical or different and are each hydrogen or halogen, Z is CH or N, m can be 1, 2, 3 or 4 and n can be 0, 1 or 2, their addition salts with acids and their metal complexes, and the preparation of these compounds, are described. The compounds are useful for treating disorders and for crop, wood and material protection.
    Type: Grant
    Filed: February 29, 1984
    Date of Patent: June 2, 1987
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Janssen, Norbert Meyer, Ernst-Heinrich Pommer, Eberhard Ammermann, Friedrich-Wilhelm Kohlmann, Walter Wesenberg, Wolfgang Heberle
  • Patent number: 4666699
    Abstract: A stain-fixative composition, for use in the microscopic identification of enteric protozoa and other parasites in fecal specimens, contains Ponceau S Stain, Chlorazol Fast Pink BK Stain, Trypan Blue Stain, dimethyl sulfoxide and a fixative component. The fixative component may be either a polyvinyl alcohol fixative or may be a mixture of isopropanol, acetic acid, liquified phenol, distilled water and optional glutaraldehyde. The stain-fixative composition is simple to prepare, has a long shelf life at ambient conditions, is easy to use and is suitable for preparing formalin or tap water concentrates, wet mount slides, or permanent smears prepared with gelatin-glycerol or resinous mounting media. In addition, the stain-fixative composition is free from the toxic mercury compounds often found in prior art staining reagents. The stain-fixative composition gives superior fixation and resolution, yet its use requires a minimum of time and attention in the laboratory.
    Type: Grant
    Filed: March 4, 1985
    Date of Patent: May 19, 1987
    Assignee: Allegheny-Singer Research Institute
    Inventor: Malcolm Slifkin
  • Patent number: 4661507
    Abstract: Compounds of the general formula: ##STR1## wherein R is naphthyl, biphenylyl, phenyl or substituted phenyl; n is 0, 1 or 2; and R.sup.1 is H, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-4 alkanoyl, or C.sub.1-2 alkyl substituted by C.sub.2-4 alkenyl with the provisos that when R.sup.1 is H or C.sub.2-4 alkanoyl, n is 0; and when n is 2, R.sup.1 is C.sub.1-3 alkyl; and their pharmaceutically acceptable salts are antifungal agents useful in combatting fungal infections in animals, including humans.
    Type: Grant
    Filed: August 28, 1984
    Date of Patent: April 28, 1987
    Assignee: Pfizer Inc.
    Inventors: Geoffrey E. Gymer, Kenneth Richardson
  • Patent number: 4658025
    Type: Grant
    Filed: December 21, 1984
    Date of Patent: April 14, 1987
    Assignee: Bayer Aktiengesellschaft
    Inventor: Fritz Maurer
  • Patent number: 4647302
    Abstract: 1-Vinyltriazole compounds of the formula ##STR1## wherein R.sup.1 is alkyl, substituted alkyl, cycloalkyl, aryl or substituted aryl;R.sup.2 is alkyl;R.sup.3 is alkyl, cycloalkyl, cycloalkenyl, substituted cycloalkenyl, alkenyl, aryl or substituted aryl; orR.sup.2 and R.sup.3, together with the carbon to which they are bonded, represent cycloalkenyl, substituted cycloalkenyl, cycloalkyl or substituted cycloalkyl;X is the group ##STR2## or, alternatively, X may represent a keto group provided that when X is a keto group R.sup.1 is alkyl, substituted alkyl, cycloalkyl, or substituted cycloalkyl;R.sup.4 is hydrogen, alkyl, aralkyl, substituted aralkyl, acyl, carbamoyl or substituted carbamoyl;R.sup.5 is hydrogen, alkyl, aralkyl or substituted aralkyl;and acid addition salts and metal salt complexes thereof; are outstandingly effective plant growth regulants and as fungicides.
    Type: Grant
    Filed: June 12, 1984
    Date of Patent: March 3, 1987
    Assignee: Bayer Aktiengesellschaft
    Inventors: Wolf Reiser, Wilfried Draber, Karl H. Buchel, Klaus Lurssen, Paul-Ernst Frohberger, Volker Paul
  • Patent number: 4639524
    Abstract: Compositions of matter are disclosed of compounds of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein X represents a halo, lower alkyl, hydrogen, trifluoromethyl, phenyl, or lower alkoxy substituent; Y represents --CN, --CONH.sub.2, --CON(R.sub.1).sub.2 or --CO.sub.2 R.sub.1 where R.sub.1 is a lower alkyl; m is the integer 1 or 2 and n is an integer from 1 to 3 inclusive; R.sub.2 represents lower alkyl; R.sub.3 represents lower alkyl or acetyl, aroyl, phenacetyl or trifluoracetyl; A, B, and D are carbonyl or methylene such that when one of A, B, or D is carbonyl, the others are methylene and R.sub.3 is lower alkyl, whereas when R.sub.3 is acetyl, aroyl, phenacetyl or trifluoroacetyl, A, B, and D are methylene. These compounds have utility as antiarrhythmic agents.
    Type: Grant
    Filed: July 9, 1984
    Date of Patent: January 27, 1987
    Assignee: G. D. Searle & Co.
    Inventors: Bipinchandra N. Desai, Robert J. Chorvat, Kurt J. Rorig
  • Patent number: 4638067
    Abstract: Novel naphthyridine-, quinoline- and benzoxazine-carboxylic acids as antibacterial agents are described as well as methods for their manufacture, formulation, and use in treating bacterial infections including the description of certain novel intermediates used in the manufacture of the antibacterial agents.
    Type: Grant
    Filed: August 12, 1985
    Date of Patent: January 20, 1987
    Assignee: Warner-Lambert Co.
    Inventors: Townley P. Culbertson, John M. Domagala, Thomas F. Mich, Jeffrey B. Nichols
  • Patent number: 4636247
    Abstract: Triazoles and imidazoles of the formula (I): ##STR1## and stereoisomers thereof, wherein W is CH or N; Q is optionally substituted aryl (especially optionally substituted phenyl), optionally substituted aralkyl, or alkyl; R.sup.1 is H, alkyl, cycloalkyl, alkenyl, alkynyl, acyl, optionally substituted aralkyl, optionally substituted phenyl, or is an alkyl or aralkyl group substituted with an ether, hydroxyl, carboxylic ester, or ketone group; R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6, which may be the same or different, are H, alkyl, cycloalkyl, optionally substituted aralkyl, or optionally substituted phenyl; and acid salts and metal complexes thereof. These compounds are useful as plant growth regulators and fungicides. Other values for R.sup.1 include C.sub.1 -C.sub.4 alkoxycarbonyl, C.sub.1 -C.sub.4 alkoxyalkyl and phenyl or benzyl substituted by benzyl.
    Type: Grant
    Filed: February 8, 1984
    Date of Patent: January 13, 1987
    Assignee: Imperial Chemical Industries PLC
    Inventors: John M. Clough, Timothy Lewis, Michael B. Gravestock
  • Patent number: 4634783
    Abstract: Amidine compounds of the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful anti-trypsin, anti-plasmin, anti-kallikrein and anti-thrombin agents. They are also useful as a powerful anti-complement agent.
    Type: Grant
    Filed: January 23, 1984
    Date of Patent: January 6, 1987
    Assignee: Torii & Co. Ltd.
    Inventors: Setsuro Fujii, Toyoo Nakayama, Shigeki Nunomura, Ryoji Matsui, Shin-ichi Watanabe, Kimio Sudo, Toshiyuki Okutome, Masateru Kurumi, Yojiro Sakurai, Takuo Aoyama
  • Patent number: 4597903
    Abstract: A process for the direct preparation of N,N-disubstituted derivatives of 4,13-diaza-18-crown-6 in which the substituents on both nitrogen atoms are identical and derive originally from an amine, by reacting a 1,8-diiodo-3,6-dioxooctane or derivatives thereof in which the substituents are located on positions 1, 2, 4, 5, 7 or 8 or combinations thereof, with a molar equivalent of a primary amine in the presence of a base and solvent.
    Type: Grant
    Filed: August 21, 1984
    Date of Patent: July 1, 1986
    Assignee: University of Maryland
    Inventors: George W. Gokel, Vincent J. Gatto